1038694-95-9Relevant academic research and scientific papers
CB 1/2 dual agonists with 3-carbamoyl 2-pyridone derivatives as antipruritics: Reduction of CNS side effects by introducing polar functional groups
Odan, Masahide,Ishizuka, Natsuki,Hiramatsu, Yoshiharu,Inagaki, Masanao,Hashizume, Hiroshi,Fujii, Yasuhiko,Mitsumori, Susumu,Morioka, Yasuhide,Soga, Masahiko,Deguchi, Masashi,Yasui, Kiyoshi,Arimura, Akinori
scheme or table, p. 2894 - 2897 (2012/06/15)
Our lead compound 1 showed high affinity for both CB1 and CB2 receptors, suggesting the possibility of inducing psychoactive side effects through the CB1 receptor in the brain. To solve this issue, polar functional groups were introduced at the 3-position of the pyridone core of compound 1 to find CB1/2 dual agonists such as 17 and 20 which did not show any CNS side effects.
Discovery of S-777469: An orally available CB2 agonist as an antipruritic agent
Odan, Masahide,Ishizuka, Natsuki,Hiramatsu, Yoshiharu,Inagaki, Masanao,Hashizume, Hiroshi,Fujii, Yasuhiko,Mitsumori, Susumu,Morioka, Yasuhide,Soga, Masahiko,Deguchi, Masashi,Yasui, Kiyoshi,Arimura, Akinori
, p. 2803 - 2806 (2012/05/20)
The discovery of novel CB2 ligands based on the 3-carbamoyl-2-pyridone derivatives by adjusting the size of side chain at 1-, 5- and 6-position is reported. The structure-activity relationship around this template lead to the identification of S-777469 as a selective CB2 receptor agonist, which exhibited the significant inhibition of scratching induced by Compound 48/80 at 1.0 mg/kg po and 10 mg/kg po (55% and 61%, respectively).
